Opinion - Switching on kinases: oncogenic activation of BRAF and the PDGFR family

Opinion - Switching on kinases: oncogenic activation of BRAF and the PDGFR family
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DOI:
10.1038/nrc1434
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发表时间:
2004-09-01
影响因子:
78.5
通讯作者:
Mol, CD
Mol, CD
中科院分区:
医学1区
文献类型:
--
作者:
Dibb, NJ;Dilworth, SM;Mol, CD

文献摘要

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血小板衍生生长因子受体(PDGFR)家族的细胞质丝氨酸/苏氨酸激酶BRAF和受体酪氨酸激酶在癌症中经常被等同氨基酸的突变激活。结构研究提供了重要的见解,为什么这些非常不同的激酶共享相似的致癌热点,为什么PDGFR质膜区域也是一个常见的致癌目标。这项研究对人类肿瘤中突变的其他激酶以及使用激酶抑制剂治疗癌症具有意义。
The cytoplasmic serine/threonine kinase BRAF and receptor tyrosine kinases of the platelet-derived growth factor receptor (PDGFR) family are frequently activated in cancer by mutations of an equivalent amino acid. Structural studies have provided important insights into why these very different kinases share similar oncogenic hot spots and why the PDGFR juxtamembrane region is also a frequent oncogenic target. This research has implications for other kinases that are mutated in human tumours and for the treatment of cancer using kinase inhibitors.